Tussionex (Hydrocodone and Phenyltoloxamine)

TUSSIONEX® Rhône-Poulenc Rorer Hydrocodone (Resin Complex)–Phenyltoloxamine (Resin Complex) Antitussive–Antihistamine

Action and Clinical

Hydrocodone is a semi-synthetic narcotic antitussive and analgesic with multiple actions qualitatively similar to those of codeine. As an antitussive, hydrocodone is approximately 3 times as potent as codeine on a weight for weight basis. The precise mechanism of action of hydrocodone and other opiates is not known; however, hydrocodone is believed to inhibit coughing by interfering with the central modulation of afferent signals, thereby decreasing sensitivity of the cough centre to incoming stimuli. In excessive doses, hydrocodone, like other opium derivatives, will depress respiration. Hydrocodone can produce miosis, euphoria, physical and psychological dependence.

Phenyltoloxamine acts as competitive inhibitor of histamine. As with other antihistamines, it is possible that its sedative and tranquilizing characteristics may contribute to its antitussive action. In addition, phenyltoloxamine in a similar manner to other antihistamines has been shown to potentiate the effects of hydrocodone.

Both of the above active ingredients are complexed to an inert cation exchange resin. It has been shown that the resin itself does not impart any additional toxicity into the final product, and the drug-resin complex produces a higher LD 50 in mice and rats for the drug substances than when they are administered in their free or common salt form. The time required to cause death in rats following a certain lethal dose of drug as an ion-exchange resin complex was longer than when the drug was administered as a soluble salt. These 2 factors combine to make these resin complexes less toxic and, hence, safer to administer orally than the soluble salt form of the drug.

The benefits derived from the sustained-release action resulting from this complexing and the apparent potentiation of the narcotic antitussive effect by phenyltoloxamine constitute the basic of action of this preparation.

Action and Clinical

The treatment of exhausting or non-productive cough; associated with cold or with upper respiratory allergic condition that does not respond to non-narcotic antitussives. It is an effective antitussive which acts for approximately 8 to 12 hours.

Contra-Indications:

Hypersensitivity to any of the components, marked hypertension, patients receiving MAO inhibitors, pre-existing respiratory depression, intracranial lesions with increased intracranial pressure.

Warnings in Clinical States:

It is important to provide appropriate therapy for the primary disease and to ensure that modification of the cough does not increase the risk of physical or psychological complications.

Children: In young children, the respiratory centre is especially susceptible to the depressant action of narcotic cough suppressants.

Pregnancy and Lactation: Since hydrocodone crosses the placenta, its use in pregnancy is not recommended. Babies of nursing mothers using opioids may become physically dependent.

Hydrocodone may inhibit peristalsis, and patients with chronic constipation should be given Tussionex only after weighing the potential therapeutic benefit against the hazards involved.

Occupational Hazards: Caution patients not to operate vehicles or hazardous machinery until their response to the drug has been determined.

Since the depressant effects of some antihistamines are additive to those of other drugs affecting the CNS, caution patients against drinking alcoholic beverages or taking hypnotics/sedatives, tricyclic antidepressants, benzodiazepines or other opiate agonists during antihistaminic therapy.

Tussionex contains hydrocodone: may be habit forming.

Tussionex suspension must not be diluted with fluids or mixed with other drugs because this alters the resin-binding and changes the absorption rate, possibly increasing the toxicity.

Precautions:

Before prescribing medication to suppress or modify cough, it is important to identify the underlying cause of the cough.

In young children, the benefit-to-risk ratio should be carefully considered, especially in children with respiratory embarrassment (e.g., croup).

Use with caution in patients with hypertension, diabetes mellitus, thyrotoxicosis, glaucoma, cardiac disease and peripheral vascular disease and in patients receiving methyldopa or beta adrenergic blockers.

The use of hydrocodone bitartrate over a prolonged period may, in susceptible individuals, lead to habituation and, in some cases, true addiction.

Adverse Reactions:

:Negligible, but when encountered may include mild constipation, nausea, facial pruritus, and drowsiness that disappear with adjustment of dose or discontinuance of treatment.

Symptoms And Treatment Of Overdose:

Symptoms: are similar to those of codeine overdosage. Narcosis is usually present, sometimes associated with convulsions. Tachycardia, bradycardia, pupillary constriction, nausea and vomiting and respiratory depression can occur. The resinated formulation mitigates the immediate absorption of large quantities of hydrocodone; however, the absorption period may be prolonged.

Treatment: If respiration is severely depressed, administer the narcotic antagonist, naloxone. Adults: 0.4 mg to 2.0 mg by i.v., i.m. or s.c. routes and repeated at 2 to 3 minute intervals if necessary. Children: 0.01 mg/kg by i.v., i.m. or s.c. routes. Dosage may be repeated also at 2 to 3 minute intervals if necessary. Since the duration of action of hydrocodone in this formulation may exceed that of naloxone, the patient should be kept under surveillance and repeated doses of naloxone should be administered as needed. Failure to obtain significant improvement after 2 to 3 doses suggests that causes other than narcotic overdosage may be responsible for the patient’s condition.

If naloxone is unsuccessful, institute intubation and respiratory support and conduct gastric lavage in the unconscious patient.

Convulsions, sometimes seen in children, can be controlled by i.v. administration of benzodiazepines (e.g., diazepam).

Dosage And Administration:

Tussionex should not be diluted with fluids or mixed with other drugs. Shake well before using.

Adults: 5 mL of suspension or 1 tablet every 8 to 12 hours. Maximum daily dose is 10 mL of suspension or 2 tablets. May be adjusted to individual requirements.

Children (Suspension): From 1 to 5 years: 2.5 mL every 12 hours (maximum daily dose of 5 mL). Over 5 years: 5 mL every 12 hours (maximum daily dose of 10 mL). Tussionex is not recommended for children under the age of 1 year or weighing less than 9 kg.

Availability And Storage:

Suspension: Each 5 mL of neutral tasting, gold-colored, thixotropic suspension, contains: hydrocodone resin.

TUSSIONEX® Rhône-Poulenc Rorer Hydrocodone (Resin Complex)–Phenyltoloxamine (Resin Complex) Antitussive–Antihistamine

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